Fig. 2: A β-lactone ligand acylates the mutant serine of K-Ras(G12S). | Nature Chemical Biology

Fig. 2: A β-lactone ligand acylates the mutant serine of K-Ras(G12S).

From: Chemical acylation of an acquired serine suppresses oncogenic signaling of K-Ras(G12S)

Fig. 2

a, Structures of β-lactones G12Si-1 and G12Si-2. b, Covalent modification of 4 µM recombinant K-Ras(G12S)•GDP or wild-type K-Ras•GDP proteins treated with 10 µM G12Si-1 or G12Si-2 assessed by whole-protein MS (n = 3). Error bars represent s.d. c, Differential scanning fluorimetry of unmodified K-Ras(G12S)•GDP and the K-Ras(G12S)•GDP•G12Si-1 complex (n = 3). d, Illustration of a biochemical assay that monitors nucleotide exchange using a fluorescent GDP analog. e, Nucleotide exchange of wild-type K-Ras, K-Ras(G12S) or K-Ras(G12S)•G12Si-1 adduct in the presence of magnesium (intrinsic), Sos or EDTA (n = 3).

Back to article page